NAS-181 (dimesylate)
CAS No. : 1217474-40-2
| Size | Price | Stock |
|---|---|---|
| 5mg | $170 | In-stock |
| 10mg | $300 | In-stock |
| 25mg | $650 | In-stock |
| 50mg | $1050 | In-stock |
| 100mg | $1850 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-103156 |
| M.Wt: | 538.63 |
| Formula: | C21H34N2O10S2 |
| Purity: | >98 % |
| Solubility: | DMSO : 62.5 mg/mL (ultrasonic) |
NAS181 is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors[1][2].
In Vitro: NAS181 has very low affinities (Ki>3000 nM) for all other receptors examined, including 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7, α1-, α2-, and β-adrenoceptors, and dopamine D1 and D2[1].
NAS181 (10-1000 nM) dose-dependently potentiates the K+-stimulated [3H]-5-HT release in preloaded rat occipital cortical slices[1].
In Vivo: NAS181 (1-10 mg/kg; s.c.) dose-dependently increases acetylcholine (ACh) release in the frontal, ventral hippocampus cortex and VHipp[1].
NAS181 (20 mg/kg; s.c.) enhances the 5-HT turnover in four rat brain regions (hypothalamus, hippocampus, striatum, and frontal cortex) with about 40%[1].
NAS181 (3 mg/kg; s.c.) produces a significant increase in the number of wet dog shakes in rats[1].
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